Patent GB-878126-A (GB)
Title: Coated medicaments
IPC: A61K9/42
Filed: 1958-04-08
Abstract: A medicament coating material comprises an intimate mixture of a non-toxic, solid fatty alcohol having from 12-31 carbon atoms or a non-toxic, solid hydroxylated fatty ester having from 12-62 carbon atoms, and a solid cellulose derivative containing no free carboxylic groups.  Preferred fatty esters include hydrogenated castor oil (principally glyceryl tri-12-hydroxystearate), glyceryl di-12-hydroxy stearate, glyceryl mono-12-hydroxy stearate, and preferred fatty alcohols include behenyl alcohol, stearyl alcohol and 12-hydroxy stearyl alcohol.  Also specified are glyceryl mono- and di-stearate, propylene glycol monolaurate, ethylene glycol monopalmitate, ethylene glycol mono-12-hydroxy stearate, glyceryl monobehenate, glyceryl monocaprate, glyceryl didecanoate, propylene glycol monomyristate, glyceryl mono-12-hydroxy stearate, glyceryl tri-12-hydroxy stearate, propylene glycol di-12-hydroxy stearate, ethylene glycol di-9, 10, -dihydroxy stearate, glyceryl tridihydroxy stearate, glyceryl mono- and di-12-hydroxy stearate, glyceryl mono-16-hydroxy stearate, glyceryl di-11-hydroxy palmitate, glyceryl tri-12-hydroxy laurate, glyceryl monostearate di-12-hydroxy stearate, propyl- and dodecyl-9, 10-dihydroxy stearates, 12-hydroxy stearyl-butyrate and palmitate, octadecyl-9, 10-dihydroxy stearate and -12-hydroxylaurate, propyl 13, 14-dihydroxy behenate, 10-hydroxy stearyl alcohol, 9, 10-dihydroxy stearyl alcohol, 14-hydroxy behenyl alcohol and lauryl, ceryl, carnaubyl, myricyl, cetyl, myristyl and arachyl alcohols. Preferred cellulose derivatives are ethyl cellulose and cellulose acetate butyrate.  Others specified are methyl- and propylcellulose, cellulose acetate, propionate, caprate, acetate-propionate and acetate-stearate.  The ratio by weight of fatty alcohol or ester to cellulosic material in the coating may be from 1 : 1-20 : 1, especially from 1 : 1 -9 : 1.  A preferred composition comprises hydrogenated castor oil and ethyl cellulose in proportions of 4 : 1. The coated medicament may be made by liquefying and admixing the fatty alcohol or ester and the cellulose derivative, either by heat or by solution in an organic solvent, e.g. chloroform and then applying the resulting coating material to the medicament.  The coating should be at least 2% by weight of the coated pellets, preferably 5%-15%.  Coated medicaments so made prolong the release of the medicament in the gastro-intestinal tract.ALSO:A medicament coating material for prolonging the release of the medicament in the gastrointestinal tract comprises an intimate mixture of a non-toxic, solid fatty alcohol having from 12-31 carbon atoms or a non-toxic, solid hydroxylated fatty ester having from 12-62 carbon atoms, and a solid cellulose derivative containing no free carboxylic groups. Preferred fatty esters include hydrogenated castor oil (principally glyceryl tri-12-hydroxystearate), glyceryl di-12-hydroxy stearate, glyceryl mono-12-hydroxy stearate, and preferred fatty alcohols include behenyl alcohol, stearyl alcohol and 12-hydroxy stearyl alcohol. Also specified are glyceryl mono- and di-stearate, propylene glycol monolaurate, ethylene glycol monopalmitate, ethylene glycol mono-12-hydroxy stearate, glyceryl monobehenate, glyceryl monocaprate, glyceryl didecanoate, propylene glycol monomyristate, glyceryl mono - 12 - hydroxy stearate, glyceryl tri-12-hydroxy stearate, propylene glycol di-12-hydroxy stearate, ethylene glycol di-9,10-dihydroxy stearate, glyceryl tridihydroxy stearate, glyceryl mono- and di-12-hydroxy stearate, glyceryl mono-16-hydroxy stearate, glyceryl di-11-hydroxy palmitate, glyceryl tri-12-hydroxy laurate, glyceryl monostearate di-12-hydroxy stearate, propyl- and dodecyl-9,10-dihydroxy stearates, 12-hydroxy stearyl-butyrate and palmitate, octadecyl-9,10-dihydroxy stearate and 12-hydroxylaurate, propyl 13,14-dihydroxy benhenate, 10-hydroxy stearyl alcohol, 9,10-dihydroxy stearyl alcohol, 14-hydroxy behenyl alcohol and lauryl, ceryl, carnaubyl, myricyl, cetyl, myristyl and arachly alcohols.  Preferred cellulose derivatives are ethyl cellulose and cellulose acetate butyrate.  Others specified are methyl- and propyl-cellulose, cellulose acetate, acetatebutyrate, propionate, caprate, acetate-propionate and acetate-stearate. The ratio by weight of fatty alcohol or ester to cellulosic material in the coating may be from 1 : 1 to 20 : 1, especially from 1 : 1 to 9 : 1.  A preferred composition comprises hydrogenated castor oil and ethyl cellulose in proportions of 4 : 1.  The coated medicament may be made by liquefying and admixing the fatty alcohol or ester and the cellulose derivative, either by heat or by solution in an organic solvent, e.g. chloroform, and then applying the resulting coating material to the medicament. The coating should be at least 2% by weight of the coated pellets, preferably 5-15%.